Assay Detail
Binding
CHEMBL861287
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Displacement of [3H]DAMGO from rat mu opioid receptor expressed in HN9.10 cells
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.63 | 8.92 |
| Ki | 9 | 7.99 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375412 | — | — | 2 | 9.29 |
| CHEMBL412331 | — | — | 2 | 9.04 |
| CHEMBL408889 | — | — | 2 | 8.28 |
| CHEMBL438739 | — | — | 2 | 7.80 |
| CHEMBL374325 | — | — | 2 | 7.70 |
| CHEMBL405192 | — | — | 2 | 7.62 |
| CHEMBL442483 | — | — | 2 | 7.58 |
| CHEMBL413644 | — | — | 2 | 7.51 |
| CHEMBL408832 | — | — | 2 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375412 | — | Ki | = | 0.51 | nM | 9.29 |
| CHEMBL412331 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL375412 | — | IC50 | = | 1.202 | nM | 8.92 |
| CHEMBL412331 | — | IC50 | = | 2.138 | nM | 8.67 |
| CHEMBL408889 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL408889 | — | IC50 | = | 10.96 | nM | 7.96 |
| CHEMBL438739 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL374325 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL405192 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL442483 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL413644 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL438739 | — | IC50 | = | 37.15 | nM | 7.43 |
| CHEMBL374325 | — | IC50 | = | 47.86 | nM | 7.32 |
| CHEMBL405192 | — | IC50 | = | 54.95 | nM | 7.26 |
| CHEMBL442483 | — | IC50 | = | 61.66 | nM | 7.21 |
| CHEMBL413644 | — | IC50 | = | 64.57 | nM | 7.19 |
| CHEMBL408832 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL408832 | — | IC50 | = | 194.98 | nM | 6.71 |